AR102967A1 - Derivados de imidazolona inhibidores de elastasas de neutrófilos humanos - Google Patents

Derivados de imidazolona inhibidores de elastasas de neutrófilos humanos

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Publication number
AR102967A1
AR102967A1 ARP150104032A ARP150104032A AR102967A1 AR 102967 A1 AR102967 A1 AR 102967A1 AR P150104032 A ARP150104032 A AR P150104032A AR P150104032 A ARP150104032 A AR P150104032A AR 102967 A1 AR102967 A1 AR 102967A1
Authority
AR
Argentina
Prior art keywords
alkyl
chr6
cycloalkyl
neutrófilos
elastasas
Prior art date
Application number
ARP150104032A
Other languages
English (en)
Inventor
Rizzi Andrea
Andrew Heald Robert
Mark Sutton Jonathan
Capaldi Carmelida
Armani Elisabetta
Original Assignee
Chiesi Farm Spa
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Chiesi Farm Spa filed Critical Chiesi Farm Spa
Publication of AR102967A1 publication Critical patent/AR102967A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D233/70—One oxygen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4178—1,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/02—Nasal agents, e.g. decongestants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/08—Bronchodilators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01—Sulfonic acids
    • C07C309/28—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C309/29—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of non-condensed six-membered aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C53/00—Saturated compounds having only one carboxyl group bound to an acyclic carbon atom or hydrogen
    • C07C53/02—Formic acid
    • C07C53/06—Salts thereof
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/04—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings

Abstract

Reivindicación 1: Un compuesto caracterizado porque es de fórmula general (1) donde A es -CH o -N-; B es -CH o -N-; D es -CH o -N-; X es -CH o -N-; R³ es -CF₃, CHF₂ o halógeno; W es un anillo heteroarilo de 5 ó 6 miembros, opcionalmente sustituido con uno o más sustituyentes seleccionados entre -CN, -NO₂, -OC₁₋₆ alquilo, -C₁₋₃ alquil-O-C₁₋₆ alquilo, -C₁₋₃ alquilamino, -C₃₋₈ cicloalquilo, -OH, C₁₋₃ alquilo, halo, -CF₃ y -SO₂C₁₋₄ alquilo; R¹ es H o se selecciona entre el grupo que consiste en -C(O)R⁴, -(CH₂)ₜ-(CHR⁶)ₙ-R⁴, -(CH₂)ₜ-(CHR⁶)ₙS(O₂)-NR⁴R⁵, -S(O₂)-R⁴, -(CH₂)ₜ-(CHR⁶)ₙ-C(O)-NR⁴R⁵, -(CH₂)ₜ-(CHR⁶)ₙ-C(O)O-R⁴; R⁴ es H o se selecciona entre el grupo que consiste en -C₁₋₆ alquilo, -C₂₋₆ alquil-NR⁷R⁸, -C₂₋₆ alquil-N⁺R⁷R⁸R⁹, -C₂₋₆ alquil-O-C₁₋₄ alquilo, -C₂₋₆ alquil-S(O₂)C₁₋₄ alquilo, -(CH₂)ₜ-arilo, -(CH₂)ₜ-C₃₋₈ cicloalquilo, -(CH₂)ₜ-C₃₋₈ heterocicloalquilo y -(CH₂)ₜ-heteroarilo, opcionalmente sustituido con uno o más sustituyentes seleccionados entre -CN, -NO₂, -OC₁₋₆ alquilo, -C₁₋₃ alquil-O-C₁₋₆ alquilo,-C₁₋₃ alquilamino, -C₃₋₈ cicloalquilo, -OH, C₁₋₃ alquilo, halo, -CF₃ y -SO₂C₁₋₄ alquilo; n es 0 o un entero seleccionado entre 1, 2 ó 3; t es 0 o un entero seleccionado entre 1, 2 ó 3; R⁵ es H o -C₁₋₆ alquilo; R⁶ es H, -C₁₋₆ alquilo, -CF₃ o -CHF₂; R⁷ es H o -C₁₋₆ alquilo; R⁸ es H o -C₁₋₆ alquilo; R⁹ es H o -C₁₋₆ alquilo; donde de manera alternativa R⁴ y R⁵ junto con él átomo de nitrógeno al cual están unidos pueden formar un sistema de anillo C₃₋₈ heterocicloalquilo o heteroarilo, opcionalmente sustituido con uno o más sustituyentes seleccionados entre -CN, -NO₂, -OC₁₋₆ alquilo, -C₁₋₃ alquil-O-C₁₋₆ alquilo, -C₁₋₃ alquilamino, -C₃₋₈ cicloalquilo, -OH, C₁₋₃ alquilo, halo, -CF₃ y -SO₂C₁₋₄ alquilo, donde los heteroátomos del sistema de anillo C₃₋₈ heterocicloalquilo o heteroarilo son un máximo de tres y se seleccionan entre -N, -NH, -O, -S- y -SO₂; R² es H o se selecciona entre el grupo que consiste de, -SMe, -S(O)R⁷, -S(O₂)R⁷ y halógeno; y sales aceptables farmacéuticamente del mismo.
ARP150104032A 2014-12-15 2015-12-10 Derivados de imidazolona inhibidores de elastasas de neutrófilos humanos AR102967A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP14198044 2014-12-15

Publications (1)

Publication Number Publication Date
AR102967A1 true AR102967A1 (es) 2017-04-05

Family

ID=52133873

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP150104032A AR102967A1 (es) 2014-12-15 2015-12-10 Derivados de imidazolona inhibidores de elastasas de neutrófilos humanos

Country Status (12)

Country Link
US (1) US9409870B2 (es)
EP (1) EP3233833B1 (es)
KR (1) KR20170095262A (es)
CN (1) CN107108577A (es)
AR (1) AR102967A1 (es)
BR (1) BR112017012608A2 (es)
CA (1) CA2970664A1 (es)
MX (1) MX2017007676A (es)
RU (1) RU2017120277A (es)
TR (1) TR201907044T4 (es)
TW (1) TW201629040A (es)
WO (1) WO2016096638A1 (es)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AR108609A1 (es) * 2016-05-31 2018-09-05 Chiesi Farm Spa Derivados de imidazolona y pirazolona como inhibidores de la elastasa de neutrófilos humana (hne)
EP3464268B1 (en) 2016-05-31 2020-03-11 Chiesi Farmaceutici S.p.A. Novel compounds
US9802919B1 (en) 2016-05-31 2017-10-31 Chiesi Farmaceutici S.P.A. Compounds

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7531560B2 (en) 2004-11-10 2009-05-12 Boehringer Ingelheim Pharmaceuticals, Inc. Anti-cytokine heterocyclic compounds
TW200808763A (en) 2006-05-08 2008-02-16 Astrazeneca Ab Novel compounds I
KR20140062476A (ko) 2011-08-01 2014-05-23 다이닛본 스미토모 세이야꾸 가부시끼가이샤 우라실 유도체 및 그 의약 용도
IN2015DN00202A (es) 2012-07-12 2015-06-12 Chiesi Farma Spa

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KR20170095262A (ko) 2017-08-22
CA2970664A1 (en) 2016-06-23
TR201907044T4 (tr) 2019-06-21
MX2017007676A (es) 2017-10-27
WO2016096638A1 (en) 2016-06-23
CN107108577A (zh) 2017-08-29
RU2017120277A (ru) 2019-01-17
EP3233833A1 (en) 2017-10-25
BR112017012608A2 (pt) 2018-01-16
US20160168101A1 (en) 2016-06-16
TW201629040A (zh) 2016-08-16
US9409870B2 (en) 2016-08-09
EP3233833B1 (en) 2019-02-20

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